alpha-Ketocarboxylic acid-based inhibitors of protein tyrosine phosphatases

Authors
Chen, YT Onaran, MB Doss, CJ Seto, CT
Citation
Yt. Chen et al., alpha-Ketocarboxylic acid-based inhibitors of protein tyrosine phosphatases, BIOORG MED, 11(14), 2001, pp. 1935-1938
Citations number
25
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
14
Year of publication
2001
Pages
1935 - 1938
Database
ISI
SICI code
0960-894X(20010723)11:14<1935:AAIOPT>2.0.ZU;2-0
Abstract
A series of aryl alpha -ketocarboxylic acids was synthesized and investigat ed as inhibitors for the protein tyrosine phosphatase from Yersinia enreroc olitica. IC50 values for these compounds range from 79 to 2700 muM. Larger aromatic groups, and aromatic groups with high electron density, lead to mo re potent inhibitors. In general, the related aryl alpha -hydroxycarboxylic acids show lower activity. (C) 2001 Elsevier Science Ltd. All rights reser ved.